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18 条记录 (耗时 0.031 秒)

    DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF
    7.
    发明申请
    DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF 有权

    公开(公告)号：US20140194470A1

    公开(公告)日：2014-07-10

    申请号：US14200698

    申请日：2014-03-07

    申请人： Jean-Michel Altenburger ,  Valerie Fossey ,  Stephane Illiano ,  Geraldine Manette

    发明人： Jean-Michel Altenburger ,  Valerie Fossey ,  Stephane Illiano ,  Geraldine Manette

    IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D491/052 ,  C07D471/04

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D471/04 ,  C07D491/052 ,  C07D495/04

    摘要： The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt: in which n is equal to 0, 1, 2, 3 or 4; m is equal to 0, 1 or 2; o is equal to 0 or 1; X represents a group —CH2, —CH(R′)—, —NH(R′)— or a heteroatom chosen from O and S, it being understood that R′ represents a group —(C1-C5)alkyl, —(C1-C5)alkoxy, —CH2-aryl, —C(O)R5 or —COOR5; R1 represents an oxo group, —COOR5, —W—OH or —W—NR5R6; R2 represents an H atom or a group chosen from the groups (i) —(C1-C5)alkyl, (ii) —(C1-C5)alkoxy, (iii) —COOR5, (iv) —NR5R6, (v) —C(O)—NR5R6, (vi) —SO2—NR3R4, (vii) heteroaryl optionally substituted with a group —(C1-C5)alkyl, (viii) —W-aryl, (ix) —W-heteroaryl, (x) —O—W-aryl, (xi) —O—W-heteroaryl and (xii) —O—W—NR5R6; it being understood that R3 and R4, (i) which may be identical or different, represent, independently of each other, an H atom, a group —(C1-C5)alkyl, —(C3-C6)cycloalkyl, aryl, heteroaryl, —CH2-heteroaryl, —(C1-C5)alkyl-NR5R6, —W—OH or —W—NR5R6; or (ii) form, together with the nitrogen atom that bears them, a heterocycloalkyl group optionally substituted with one or more groups chosen from the groups —(C1-C5)alkyl and —CH2-aryl; W is a group —(C1-C5)alkylene, optionally substituted with one or more hydroxyl groups; R5 and R6, which may be identical or different, represent, independently of each other, a hydrogen atom or a group chosen from the groups —(C1-C5)alkyl and the groups —(C3-C6)cycloalkyl, and also the process for preparing them and the therapeutic uses thereof.

    Chlorothiophene-isoxazoles as inhibitors of coagulation factors Xa and thrombin
    9.
    发明授权
    Chlorothiophene-isoxazoles as inhibitors of coagulation factors Xa and thrombin 有权
    氯噻吩 - 异恶唑作为凝血因子Xa和凝血酶的抑制剂

    公开(公告)号：US08835653B2

    公开(公告)日：2014-09-16

    申请号：US12858981

    申请日：2010-08-18

    申请人： Markus Follmann ,  Volkmar Wehner ,  Jean-Michel Altenburger ,  Gilbert Lassalle ,  Jean-Pascal Herault

    发明人： Markus Follmann ,  Volkmar Wehner ,  Jean-Michel Altenburger ,  Gilbert Lassalle ,  Jean-Pascal Herault

    IPC分类号： C07D413/14 ,  A61K31/55 ,  A61P9/10 ,  A61P7/02 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D413/04

    CPC分类号： C07D413/14 ,  C07D413/04

    摘要： The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 本发明涉及式I化合物，其中R1; R2; R3; R4; R5，R16，X和M具有权利要求中所示的含义。 式I的化合物是有价值的药理活性化合物。 它们表现出强烈的抗血栓形成作用，并且适用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa和凝血酶的可逆抑制剂，并且通常可用于存在因子Xa和/或凝血酶的不期望活性或用于治疗或预防因子Xa和凝血酶的抑制的病症 是打算的 本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

    N-(heterocyclyl)benzene or pyridinesulphonamides as antithrombotic agents and anticoagulants
    10.
    发明授权
    N-(heterocyclyl)benzene or pyridinesulphonamides as antithrombotic agents and anticoagulants 失效
    N-（杂环基）苯或吡啶磺酰胺作为抗血栓剂和抗凝剂

    公开(公告)号：US06680329B2

    公开(公告)日：2004-01-20

    申请号：US10221404

    申请日：2002-09-12

    申请人： Jean-Michel Altenburger ,  Gérard Cremer ,  Gilbert Lassalle ,  Mostafa Matrougui

    发明人： Jean-Michel Altenburger ,  Gérard Cremer ,  Gilbert Lassalle ,  Mostafa Matrougui

    IPC分类号： A61K31445

    CPC分类号： C07D213/73 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D409/14 ,  Y02P20/55

    摘要： Compounds of formula [I] in which: W may represent a —(CH2)2—, —(CH2)3—, —CH2—C≡C— or —CH2—CH═CH— group, R2 may in particular represent a piperidyl group, an optionally substituted 1,2,3,6-tetrahydropyridyl group, a hexahydro-1H-azepinyl group, an optionally substituted piperazinyl group or a morpholinyl group, R3 may in particular represent a group —COR1, A may in particular represent an optionally substituted phenyl group, a heterocycle or a cyclopentyl group, and B may in particular represent a pyridyl group, an aminopyrazinyl group, an aminopyridazinyl group, a pyrimidinyl group optionally substituted with an amino group, piperidyl group or an aminopyridyl group optionally substituted on the pyridine with a (C1-C4)alkyl or (C1-C4)alkoxy group, the amino group possibly also being substituted with a (C1-C4)alkyl group, their preparation and their therapeutic application.

    摘要翻译： 式[I]化合物其中：W可以表示 - （CH 2）2 - ， - （CH 2）3 - ， - CH 2 -C = C-或-CH 2 -CH = CH-基团，R 2可以特别地表示 哌啶基，任选取代的1,2,3,6-四氢吡啶基，六氢-1H-吖庚因基，任选取代的哌嗪基或吗啉基，R 3可特别表示基团-COR 1，A可特别表示 任选取代的苯基，杂环或环戊基，B可特别表示吡啶基，氨基吡嗪基，氨基哒嗪基，任选被氨基取代的嘧啶基，哌啶基或任选取代的氨基吡啶基 吡啶与（C1-C4）烷基或（C1-C4）烷氧基，氨基也可能被（C1-C4）烷基取代，其制备及其治疗应用。